The role of alpha(2)-adrenoceptors in mediating the noradrenergic cont
rol of female sexual behaviour was investigated employing a selective
alpha(2)-adrenoceptor antagonist, delequamine (RS15385). The drug was
given in graded doses of 0.01-30 mg/kg p.o. to ovariectomised plus adr
enalectomised rats primed with either 2 mu g oestradiol benzoate which
yielded mainly non-receptive animals or 5 mu g oestradiol benzoate fo
llowed 48 h later by 0.5 mg progesterone, which stimulated a high leve
l of receptivity. Doses between 0.1 and 30 mg/kg significantly increas
ed lordotic activity (receptivity) with an ED(50) of 0.32 mg/kg, but h
ad no effect on ear-wiggling or hopping-and-darting (proceptivity). De
lequamine had no inhibitory effect in animals displaying high levels o
f receptivity. Thus we have shown a selective alpha(2)-adrenoceptor an
tagonist, given orally, can stimulate female receptivity in a dose-dep
endent manner. Bilateral administration into the ventromedial nucleus,
but not medial preoptic area, of delequamine (10 mu g/side/rat) stimu
lated receptivity and it is suggested that the alpha(2)-adrenoceptor m
ay exert its effect by enhancing endogenous noradrenaline release at i
ts active sites.